Synthesis and biological evaluation of coumarin-quinone hybrids as multifunctional bioactive agents

Authors

  • Anees Pangal Dept. of Chemistry & Post Graduate Centre, Abeda Inamdar Sr. College of Arts, Science & Commerce, Camp, Pune – 411001, India https://orcid.org/0000-0002-3406-6839
  • Khursheed Ahmed Dept. of Chemistry & Post Graduate Centre, Abeda Inamdar Sr. College of Arts, Science & Commerce (Autonomous), Camp, Pune – 411001, India https://orcid.org/0000-0003-0751-6790

DOI:

https://doi.org/10.5599/admet.1468
coumarin-quinone hybrids

Abstract

We report the synthesis, structural characterization and pharmaceutical activity of four coumarin-quinone hybrids. The compounds were significantly active against Staphylococcus aureus, Pseudomonas aeoginosa and Candida albicans. Promising antioxidant activity was observed when compared to ascorbic acid. Two compounds, DTBSB and DTBSN, also showed commendable in vitro antiproliferative activities against the cells of human cancer cell lines MCF-7, MDA-MB-231, COLO-205, HT-29 and A549 along with appreciable tumor selectivity with distinct selectivity index. Molecular docking studies using cyclooxygenase-2 (PDB ID: 6COX) revealed strong binding affinities for the COX-2 active site. Moreover, ADMET properties of the synthesized compounds were determined using the pKCSM and SwissADME online tools and all the compounds had accurate pharmacokinetic profiles. Hence, the new coumarin-quinone hybrids DTBSB and DTBSN can be considered for optimization and lead development.

 

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Published

07-10-2022

How to Cite

Pangal, A., & Ahmed, K. (2022). Synthesis and biological evaluation of coumarin-quinone hybrids as multifunctional bioactive agents. ADMET and DMPK, 11(1), 81–96. https://doi.org/10.5599/admet.1468

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Section

Original Scientific Articles